WO2009076408A3 - 3 -carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists - Google Patents
3 -carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists Download PDFInfo
- Publication number
- WO2009076408A3 WO2009076408A3 PCT/US2008/086171 US2008086171W WO2009076408A3 WO 2009076408 A3 WO2009076408 A3 WO 2009076408A3 US 2008086171 W US2008086171 W US 2008086171W WO 2009076408 A3 WO2009076408 A3 WO 2009076408A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- opioid receptor
- carboxypropyl
- compounds
- receptor antagonists
- aminotetralin derivatives
- Prior art date
Links
- 102000051367 mu Opioid Receptors Human genes 0.000 title abstract 3
- 108020001612 μ-opioid receptors Proteins 0.000 title abstract 3
- CWIYTZKBIVONFO-UHFFFAOYSA-N 4-(1-amino-3,4-dihydro-2h-naphthalen-1-yl)butanoic acid Chemical class C1=CC=C2C(N)(CCCC(O)=O)CCCC2=C1 CWIYTZKBIVONFO-UHFFFAOYSA-N 0.000 title abstract 2
- 229940123257 Opioid receptor antagonist Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000005557 antagonist Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/48—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring being part of a condensed ring system of the same carbon skeleton
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C215/64—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/28—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T436/00—Chemistry: analytical and immunological testing
- Y10T436/17—Nitrogen containing
- Y10T436/173845—Amine and quaternary ammonium
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Pulmonology (AREA)
- Otolaryngology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Inorganic Chemistry (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Priority Applications (10)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
NZ586048A NZ586048A (en) | 2007-12-11 | 2008-12-10 | 3 -carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists |
CA2707981A CA2707981C (en) | 2007-12-11 | 2008-12-10 | 3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists |
CN200880119873.7A CN101896455B (en) | 2007-12-11 | 2008-12-10 | 3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists |
EP08859864A EP2231585B1 (en) | 2007-12-11 | 2008-12-10 | 3-carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists |
RU2010128542/04A RU2482107C2 (en) | 2007-12-11 | 2008-12-10 | 3-carboxypropyl-aminotetraline derivatives and related compounds as mu-opioid receptor antagonists |
ES08859864T ES2402749T3 (en) | 2007-12-11 | 2008-12-10 | 3-Carboxypropyl-aminotetralin derivatives as opioid receptor antagonists mu |
AU2008335210A AU2008335210B2 (en) | 2007-12-11 | 2008-12-10 | 3 -carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists |
BRPI0821611A BRPI0821611A8 (en) | 2007-12-11 | 2008-12-10 | 3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVE AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS |
JP2010538112A JP5403762B2 (en) | 2007-12-11 | 2008-12-10 | 3-Carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists |
IL205949A IL205949A (en) | 2007-12-11 | 2010-05-25 | 3-carboxypropyl-aminotetralin derivatives and related compounds, pharmaceutical compositions comprising the same, a process for their preparation and uses thereof |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US722007P | 2007-12-11 | 2007-12-11 | |
US61/007,220 | 2007-12-11 | ||
US4921908P | 2008-04-30 | 2008-04-30 | |
US61/049,219 | 2008-04-30 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2009076408A2 WO2009076408A2 (en) | 2009-06-18 |
WO2009076408A3 true WO2009076408A3 (en) | 2009-09-03 |
Family
ID=40521484
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US2008/086171 WO2009076408A2 (en) | 2007-12-11 | 2008-12-10 | 3 -carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists |
Country Status (18)
Country | Link |
---|---|
US (5) | US8106232B2 (en) |
EP (1) | EP2231585B1 (en) |
JP (1) | JP5403762B2 (en) |
KR (1) | KR101610165B1 (en) |
CN (1) | CN101896455B (en) |
AR (1) | AR072336A1 (en) |
AU (1) | AU2008335210B2 (en) |
BR (1) | BRPI0821611A8 (en) |
CA (1) | CA2707981C (en) |
CL (1) | CL2008003672A1 (en) |
CO (1) | CO6300937A2 (en) |
ES (1) | ES2402749T3 (en) |
IL (1) | IL205949A (en) |
MY (1) | MY149973A (en) |
NZ (1) | NZ586048A (en) |
RU (1) | RU2482107C2 (en) |
TW (1) | TWI412360B (en) |
WO (1) | WO2009076408A2 (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8183274B2 (en) | 2005-05-13 | 2012-05-22 | The Regents Of The University Of California | Treatment of hyperproliferative disorders with diarylhydantoin compounds |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2449993C2 (en) | 2006-03-29 | 2012-05-10 | Те Риджентс Оф Те Юниверсити Оф Калифорния | Diarylthiohydatoic compounds |
CA2966280A1 (en) | 2007-10-26 | 2009-04-30 | The Regents Of The University Of California | Diarylhydantoin compounds |
ES2402748T3 (en) | 2007-12-11 | 2013-05-08 | Theravance, Inc. | Aminotetralin compounds as opioid receptor antagonists mu |
US8153686B2 (en) | 2008-04-01 | 2012-04-10 | Theravance, Inc. | Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists |
AU2009324709B2 (en) | 2008-12-10 | 2015-07-16 | Theravance Biopharma R&D Ip, Llc | Crystalline forms of a 3-carboxypropyl-aminotetralin compound |
NZ598783A (en) * | 2009-09-18 | 2013-07-26 | Adolor Corp | Use of opioid receptor antagonist for gastrointestinal tract disorders |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000037426A1 (en) * | 1998-12-22 | 2000-06-29 | Astrazeneca Ab | Novel oxo-aminotetralin compounds useful in pain management |
US6498196B1 (en) * | 1998-12-22 | 2002-12-24 | Edward Roberts | Compounds useful in pain management |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2123500T3 (en) * | 1989-05-31 | 1999-01-16 | Upjohn Co | DERIVATIVES OF 8-HETEROCICLIL-2-AMINOTETRALINA ACTIVE ON THE CENTRAL NERVOUS SYSTEM. |
AU3092800A (en) * | 1998-12-22 | 2000-07-12 | Astra Pharma Inc. | Novel thio-aminotetralin compounds useful in pain management |
US6844368B1 (en) * | 1998-12-22 | 2005-01-18 | Edward Roberts | Compounds useful in pain management |
US6231594B1 (en) * | 1999-08-11 | 2001-05-15 | Radiant Medical, Inc. | Method of controlling body temperature while reducing shivering |
JP2010509227A (en) | 2006-11-07 | 2010-03-25 | ネクター セラピューティックス エイエル,コーポレイション | Opioid agonist and opioid antagonist dosage forms and co-administration |
ES2402748T3 (en) * | 2007-12-11 | 2013-05-08 | Theravance, Inc. | Aminotetralin compounds as opioid receptor antagonists mu |
US8153686B2 (en) | 2008-04-01 | 2012-04-10 | Theravance, Inc. | Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists |
AU2009324709B2 (en) | 2008-12-10 | 2015-07-16 | Theravance Biopharma R&D Ip, Llc | Crystalline forms of a 3-carboxypropyl-aminotetralin compound |
-
2008
- 2008-12-10 TW TW097148045A patent/TWI412360B/en not_active IP Right Cessation
- 2008-12-10 NZ NZ586048A patent/NZ586048A/en not_active IP Right Cessation
- 2008-12-10 ES ES08859864T patent/ES2402749T3/en active Active
- 2008-12-10 JP JP2010538112A patent/JP5403762B2/en not_active Expired - Fee Related
- 2008-12-10 MY MYPI2010002437A patent/MY149973A/en unknown
- 2008-12-10 RU RU2010128542/04A patent/RU2482107C2/en active
- 2008-12-10 US US12/331,659 patent/US8106232B2/en not_active Expired - Fee Related
- 2008-12-10 EP EP08859864A patent/EP2231585B1/en active Active
- 2008-12-10 CL CL2008003672A patent/CL2008003672A1/en unknown
- 2008-12-10 CA CA2707981A patent/CA2707981C/en active Active
- 2008-12-10 KR KR1020107014774A patent/KR101610165B1/en active IP Right Grant
- 2008-12-10 AR ARP080105365A patent/AR072336A1/en unknown
- 2008-12-10 AU AU2008335210A patent/AU2008335210B2/en not_active Ceased
- 2008-12-10 BR BRPI0821611A patent/BRPI0821611A8/en not_active Application Discontinuation
- 2008-12-10 CN CN200880119873.7A patent/CN101896455B/en not_active Expired - Fee Related
- 2008-12-10 WO PCT/US2008/086171 patent/WO2009076408A2/en active Application Filing
-
2010
- 2010-05-25 IL IL205949A patent/IL205949A/en active IP Right Grant
- 2010-06-11 CO CO10070802A patent/CO6300937A2/en not_active Application Discontinuation
-
2011
- 2011-12-19 US US13/330,363 patent/US8318765B2/en active Active
-
2012
- 2012-10-16 US US13/652,808 patent/US8492399B2/en active Active
-
2013
- 2013-06-19 US US13/921,448 patent/US8703791B2/en active Active
-
2014
- 2014-03-04 US US14/196,186 patent/US8969370B2/en not_active Expired - Fee Related
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000037426A1 (en) * | 1998-12-22 | 2000-06-29 | Astrazeneca Ab | Novel oxo-aminotetralin compounds useful in pain management |
US6498196B1 (en) * | 1998-12-22 | 2002-12-24 | Edward Roberts | Compounds useful in pain management |
Non-Patent Citations (2)
Title |
---|
GRUNDT, P. ET AL.: "Identification of a new scaffold for opioid receptor antagonism based on the 2-amino-1,1-dimethyl-7-hydroxytetralin pharmacophore", J. MED. CHEM., vol. 47, no. 21, 2004, pages 5069 - 5075, XP002535832 * |
ROY, C. ET AL.: "Synthesis and structure-activity relationship of novel aminotetralin derivatives with high mu selective opioid affinity", BIOORG. MED. CHEM. LETTERS, vol. 12, no. 21, 2002, pages 3141 - 3143, XP002535833 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8183274B2 (en) | 2005-05-13 | 2012-05-22 | The Regents Of The University Of California | Treatment of hyperproliferative disorders with diarylhydantoin compounds |
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